Terbinafine-loaded biocompatible hydrogel patches composed of hydroxyethyl methacrylate and methacrylic acid with remarkable antifungal activities

IF 3.4 4区 工程技术 Q2 POLYMER SCIENCE
Kemal Çetin, Koray Şarkaya, Fatih Altıntaş, Berna Kavakcıoğlu Yardımcı
{"title":"Terbinafine-loaded biocompatible hydrogel patches composed of hydroxyethyl methacrylate and methacrylic acid with remarkable antifungal activities","authors":"Kemal Çetin,&nbsp;Koray Şarkaya,&nbsp;Fatih Altıntaş,&nbsp;Berna Kavakcıoğlu Yardımcı","doi":"10.1007/s13233-025-00379-6","DOIUrl":null,"url":null,"abstract":"<div><p>Oral administration of terbinafine hydrochloride for the treatment of superficial mycoses in the targeted skin area may require high concentrations due to first-pass metabolism and intensive plasma protein binding. To address these challenges, this study aimed to fabricate hydrogel patches for localized delivery of terbinafine hydrochloride. The patches were developed using methacrylic acid and 2-hydroxyethyl methacrylate monomers through a free radical polymerization technique. Infrared spectroscopy, field emission scanning electron microscopy, and time-dependent swelling tests were performed to examine the physicochemical, structural, and morphological characteristics of hydrogel patches. Hydrogels exhibit interconnected highly porous structures suitable for drug loading and controlled release. Biocompatibility was assessed through in vitro cytotoxicity and comet assays, showing no significant cytotoxic or genotoxic effects on human embryonic kidney cells, even at high extract concentrations. Terbinafine was loaded into biocompatible hydrogels with different monomer ratios, and it was found that both the loading content (from 3.84 to 5.83%) and the entrapment efficiency (from 26.63 to 41.45%) increased as the methacrylic acid composition increased. These patches can release the drug at higher concentrations depending on their methacrylic acid content while retaining the drug's inhibitory action on yeast microbiological growth. These findings suggest that the developed hydrogel patches could serve as efficient platforms for topical antifungal therapy following further clinical studies.</p><h3>Graphical abstract</h3>\n<div><figure><div><div><picture><source><img></source></picture></div><div><p>Hydrogel patches with antifungal activities</p></div></div></figure></div></div>","PeriodicalId":688,"journal":{"name":"Macromolecular Research","volume":"33 7","pages":"911 - 920"},"PeriodicalIF":3.4000,"publicationDate":"2025-03-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s13233-025-00379-6.pdf","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Macromolecular Research","FirstCategoryId":"5","ListUrlMain":"https://link.springer.com/article/10.1007/s13233-025-00379-6","RegionNum":4,"RegionCategory":"工程技术","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"POLYMER SCIENCE","Score":null,"Total":0}
引用次数: 0

Abstract

Oral administration of terbinafine hydrochloride for the treatment of superficial mycoses in the targeted skin area may require high concentrations due to first-pass metabolism and intensive plasma protein binding. To address these challenges, this study aimed to fabricate hydrogel patches for localized delivery of terbinafine hydrochloride. The patches were developed using methacrylic acid and 2-hydroxyethyl methacrylate monomers through a free radical polymerization technique. Infrared spectroscopy, field emission scanning electron microscopy, and time-dependent swelling tests were performed to examine the physicochemical, structural, and morphological characteristics of hydrogel patches. Hydrogels exhibit interconnected highly porous structures suitable for drug loading and controlled release. Biocompatibility was assessed through in vitro cytotoxicity and comet assays, showing no significant cytotoxic or genotoxic effects on human embryonic kidney cells, even at high extract concentrations. Terbinafine was loaded into biocompatible hydrogels with different monomer ratios, and it was found that both the loading content (from 3.84 to 5.83%) and the entrapment efficiency (from 26.63 to 41.45%) increased as the methacrylic acid composition increased. These patches can release the drug at higher concentrations depending on their methacrylic acid content while retaining the drug's inhibitory action on yeast microbiological growth. These findings suggest that the developed hydrogel patches could serve as efficient platforms for topical antifungal therapy following further clinical studies.

Graphical abstract

Hydrogel patches with antifungal activities

由甲基丙烯酸羟乙酯和甲基丙烯酸组成的特比萘芬生物相容性水凝胶片具有显著的抗真菌活性
口服盐酸特比萘芬治疗目标皮肤浅表真菌病,由于首过代谢和血浆蛋白结合强烈,可能需要高浓度的盐酸特比萘芬。为了解决这些挑战,本研究旨在制造用于盐酸特比萘芬局部递送的水凝胶贴片。以甲基丙烯酸和甲基丙烯酸2-羟乙基单体为原料,通过自由基聚合技术制备了贴片。通过红外光谱、场发射扫描电镜和随时间变化的溶胀测试来检测水凝胶贴片的物理化学、结构和形态特征。水凝胶具有相互连接的高多孔结构,适合于药物装载和控制释放。通过体外细胞毒性和彗星试验评估生物相容性,显示即使在高浓度提取物下,对人类胚胎肾细胞也没有显著的细胞毒性或基因毒性作用。将特比萘芬以不同单体比例加载到生物相容性水凝胶中,发现随着甲基丙烯酸组分的增加,负载含量(从3.84增加到5.83%)和包封效率(从26.63增加到41.45%)均有所增加。这些贴片可以根据其甲基丙烯酸含量以更高的浓度释放药物,同时保留药物对酵母微生物生长的抑制作用。这些发现表明,在进一步的临床研究中,开发的水凝胶贴片可以作为局部抗真菌治疗的有效平台。图片摘要:具有抗真菌活性的水凝胶贴片
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 求助全文
来源期刊
Macromolecular Research
Macromolecular Research 工程技术-高分子科学
CiteScore
4.70
自引率
8.30%
发文量
100
审稿时长
1.3 months
期刊介绍: Original research on all aspects of polymer science, engineering and technology, including nanotechnology Presents original research articles on all aspects of polymer science, engineering and technology Coverage extends to such topics as nanotechnology, biotechnology and information technology The English-language journal of the Polymer Society of Korea Macromolecular Research is a scientific journal published monthly by the Polymer Society of Korea. Macromolecular Research publishes original researches on all aspects of polymer science, engineering, and technology as well as new emerging technologies using polymeric materials including nanotechnology, biotechnology, and information technology in forms of Articles, Communications, Notes, Reviews, and Feature articles.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信